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Cetirizine

CHEMBL1000 Phase 4 Approuvé Small molecule
Half-Life
6.5-10 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
388.9 g/mol
LogP
1.7
Phase
4

A second-generation antihistamine that selectively blocks peripheral H1 receptors to relieve symptoms of allergic rhinitis, chronic urticaria, and other allergic conditions. Unlike first-generation antihistamines, it has low CNS penetration, resulting in less sedation in most patients. It is available over the counter and is one of the most widely used allergy medications worldwide.

Masse moléculaire

388,8900 g/mol

LogP

1,70

TPSA

53,00 Ų

Règle des 5 de Lipinski

Conforme

Aires thérapeutiques

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Non-Small Cell Lung Cancer Asthma Migraine Schizophrenia Multiple Sclerosis Oncology Type 2 Diabetes Breast Cancer Atopic Dermatitis Prostate Cancer Colorectal Cancer

Classes de médicaments

R — R - Respiratory System

Mécanisme d'action

Second-generation H1 antihistamine.

Pharmacokinetics (PK)

Half-Life 6.5-10 hours

Pharmacodynamics (PD)

Mécanisme

Second-generation H1 antihistamine.

Structure 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
O=C(O)COCCN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1

                

                

                
                

                    
InChI

                    
InChI=1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26)

                

                

                

                    
                    

                        
Molecular Formula

                        
C21H25ClN2O3

                    

                    
                    

                        
HBD / HBA

                        
1 / 5

                    

                    
                    

                        
Liaisons Rotatives

                        
8

                    

                    
                    
                    

                        
Atomes Lourds

                        
27

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            HRH1 (Histamine H1 Receptor)
                            Antagonist
                        

                        
                        Primary Target
                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Moderate


                            
                                Cetirizine + Oxycodone
                            
                        

                        
                        
Concurrent use of cetirizine and oxycodone may produce additive CNS and respiratory depression, increasing the risk of sedation and, at higher doses, respiratory compromise.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Cetirizine + Morphine
                            
                        

                        
                        
Cetirizine may add to morphine-induced CNS depression, increasing sedation and potentially enhancing respiratory depression, particularly with higher doses of either agent.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Cetirizine + Alprazolam
                            
                        

                        
                        
Cetirizine has mild CNS depressant properties that can be additive with the sedative effects of alprazolam, increasing the risk of excessive sedation, psychomotor impairment, and respiratory depression.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Foire aux questions

                

                    
                    

                        
                        

                            
A second-generation antihistamine that selectively blocks peripheral H1 receptors to relieve symptoms of allergic rhinitis, chronic urticaria, and other allergic conditions. Unlike first-generation antihistamines, it has low CNS penetration, resulting in less sedation in most patients. It is available over the counter and is one of the most widely used allergy medications worldwide.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Second-generation H1 antihistamine.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Cetirizine: Half-life: 6.5-10 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Cetirizine is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Albuterol
                            Small molecule
                        
                        
                        
                            Montelukast
                            Small molecule
                        
                        
                        
                            Loratadine
                            Small molecule
                        
                        
                        
                            Diphenhydramine
                            Small molecule
                        
                        
                    

                

                

                
                
                
            

            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL1000.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 2678.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
Avertissement médical

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.